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PHA-793887
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PHA-793887图片
CAS NO:718630-59-2
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
2mg电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
PHA-793887 是一种有效的,ATP 竞争性的CDK抑制剂,可抑制 Cdk2,Cdk1,Cdk4 和 Cdk9 的活性,IC50值分别为 8 nM,60 nM,62 nM 和 138 nM,同时可抑制糖原合酶激酶 3β (GSK-3β),IC50值为 79 nM。
生物活性

PHA-793887 is a potent, ATP-competitiveCDKinhibitor, can inhibitCdk2,Cdk1,Cdk4, andCdk9withIC50s of 8 nM, 60 nM, 62 nM and 138 nM, respectively, and also inhibits glycogen synthase kinase 3β with anIC50of 79 nM.

IC50& Target[4]

Cdk5/p25

5 nM (IC50)

cdk2/cyclin A

8 nM (IC50)

CDK2/cyclinE

8 nM (IC50)

CDK7/cyclin H

10 nM (IC50)

Cdk1/cyclin B

60 nM (IC50)

Cdk4/cyclin D1

62 nM (IC50)

CDK9/cyclinT1

138 nM (IC50)

GSK-3β

79 nM (IC50)

体外研究
(In Vitro)

PHA-793887 partially inhibits Rb phosphorylation at 1 μM and almost completely at 3 μM, in A2780 tumor cell line. PHA-793887 (1 μM) partially inhibits phosphorylation of the Cdk2 substrates Rb and NPM in A2780 tumor cell line. PHA-793887 (6 μM) significantly inhibits Rb and NPM phosphorylation in MCF7 cell line[1]. PHA-793887 shows cytotoxic activities against leukemic cell lines in vitro, with IC50ranging from 0.3 to 7 μM. In colony assays, PHA-793887 is highly cytotoxic for leukemia cell lines, with an IC50<0.1 μM. PHA-793887 induces cell-cycle arrest, inhibits Rb and nucleophosmin phosphorylation, and modulates cyclin E and cdc6 expression at low doses of 0.2 to 1 μM and induces apoptosis at the highest dose of 5 μM. PHA-793887 is a novel inhibitor of several cdk, including cdk1, cdk2, cdk4, cdk5, cdk7, and cdk9 with IC50in the 5 to 140 nM range[3].

体内研究
(In Vivo)

PHA-793887 induces tumor growth inhibition in the range of 50% at dose of 15 mg/kg to 75% at dose of 30 mg/kg in CD-1 nude mice. PHA-793887 (30 mg/kg, i.v.) also induces significant downregulation of the 58-gene panel in the skin of CD-1 mice[1]. PHA-793887 (20 mg/kg, i.v.) induces tumor regression in the HL60 model. In the K562 model, PHA-793887 significantly reduces tumor growth. Moreover, PHA-793887 (20 mg/kg, i.v.) inhibits human primary leukemia growth in engraftment setting in vivo[3].

Clinical Trial
分子量

361.48

性状

Solid

Formula

C19H31N5O2

CAS 号

718630-59-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : ≥ 50 mg/mL(138.32 mM)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.7664 mL13.8320 mL27.6640 mL
5 mM0.5533 mL2.7664 mL5.5328 mL
10 mM0.2766 mL1.3832 mL2.7664 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 2.5 mg/mL (6.92 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.92 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在本网站选购。